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质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
NC1=CC=CC(S(N2CCN(S(C3=CC=C(OCCO4)C4=C3)(=O)=O)CCC2)(=O)=O)=C1
InChI
1S/C19H23N3O6S2/c20-15-3-1-4-16(13-15)29(23,24)21-7-2-8-22(10-9-21)30(25,26)17-5-6-18-19(14-17)28-12-11-27-18/h1,3-6,13-14H,2,7-12,20H2
InChI key
GMHIOMMKSMSRLY-UHFFFAOYSA-N
生化/生理作用
DASA-58 is a potent and selective activator of cancer-specific pyruvate kinase isoform PKM2 (hPKM2 AC50 = 38 nM, Emax = 82%), but not PKM1, PKR or PKL, that stabilizes PKM2 tetrameric conformation by targeting a site distinct from that of fructose-1,6-bis-phosphate (FBP). DASA-58 exhibits good aqueous solubility (51.2 μg/mL), decreases cellular lactate production and suppresses cell proliferation selectively under hypoxic conditions (30 μM; H1299, 1% O2). When administered in mice, DASA-58 is reported to exhibit anti-thrombotic efficacy in vivo (40 mg/kg via iv).
Potent and selective activator of cancer-specific pyruvate kinase PKM2 in vitro and in vivo, but not PKM1, PKR or PKL.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
Qiuyue Kong et al.
Diabetes, 68(2), 361-376 (2018-11-21)
Nonalcoholic steatohepatitis (NASH) is the most prevalent cause of chronic liver disease worldwide. Macrophage-mediated inflammation plays a critical role in NASH pathogenesis; however, optimum therapies for macrophage activation and NASH remain elusive. HSPA12A encodes a novel member of the HSP70
Xinxing Ouyang et al.
Journal of molecular cell biology, 11(2), 93-106 (2018-11-15)
Glucose metabolism plays a key role in thymocyte development. The mammalian target of rapamycin complex 2 (mTORC2) is a critical regulator of cell growth and metabolism, but its role in early thymocyte development and metabolism has not been fully studied.
Matthew B Boxer et al.
Journal of medicinal chemistry, 53(3), 1048-1055 (2009-12-19)
The metabolism of cancer cells is altered to support rapid proliferation. Pharmacological activators of a tumor cell specific pyruvate kinase isozyme (PKM2) may be an approach for altering the classic Warburg effect characteristic of aberrant metabolism in cancer cells yielding
Elisa Monzón-Casanova et al.
Nature immunology, 19(3), 267-278 (2018-01-24)
Antibody affinity maturation occurs in germinal centers (GCs), where B cells cycle between the light zone (LZ) and the dark zone. In the LZ, GC B cells bearing immunoglobulins with the highest affinity for antigen receive positive selection signals from
Andrew Leber et al.
Inflammatory bowel diseases, 24(9), 1978-1991 (2018-05-03)
Inflammatory bowel disease (IBD) afflicts 5 million people and is increasing in prevalence. There is an unmet clinical need for safer and effective treatments for IBD. The BT-11 is a small molecule oral therapeutic that ameliorates IBD by targeting lanthionine
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